Bupropion: 6 things you should know
Medically reviewed by C. Fookes, BPharm Last updated on Oct 29, 2018.
1. How it works
- Bupropion is an antidepressant that may also be used to help people quit smoking.
- Experts aren't exactly sure how bupropion works in depression but presume it is due to its ability to inhibit the reuptake of two neurotransmitters, norepinephrine, and dopamine (although this reuptake inhibition is weak). Bupropion does not affect the reuptake of serotonin or inhibit monoamine oxidase.
- Bupropion is thought to be effective for smoking cessation because of its ability to increase dopamine levels in the nerve synapse by inhibiting the reuptake of dopamine. This replaces the dopamine deficiency experienced during nicotine withdrawal (nicotine causes a release of dopamine which enhances the pleasure-seeking pathways in the brain; reducing nicotine intake means these pathways are no longer being stimulated; bupropion counteracts this effect).
- Bupropion is an aminoketone antidepressant and is chemically unrelated to any other type of antidepressant.
- Bupropion (Wellbutrin and Aplenzin brands, generic bupropion) may be used to relieve the symptoms of depression in Major Depressive Disorder (MDD) and Seasonal Affective Disorder (SAD).
- Bupropion (Zyban brand, generic bupropion) may be used to relieve cravings associated with nicotine withdrawal during smoking cessation. Research has shown that treatment with Zyban is significantly more effective at helping people to quit smoking than no treatment. Zyban may also be combined with a Nicotine Transdermal System (nicotine patches), although blood pressure should be monitored.
- Generic bupropion is available and bupropion is also marketed under the brand names Wellbutrin and Aplenzin (both for depression) and Zyban (for smoking cessation).
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Insomnia, headache, dizziness, dry mouth, sore throat, nausea, and constipation are the more commonly reported side effects. May also cause abdominal pain, abnormal dreams, flushing, muscle and joint pain, migraine, rash or an itchy skin.
- Severe neuropsychiatric symptoms, including agitation, anxiety, delusions, hallucinations, panic disorder, paranoia, and psychosis have been reported with bupropion use. These have occurred in people with and without pre-existing psychiatric disease. People should be monitored for the appearance of neuropsychiatric symptoms. Most cases resolved on discontinuation of bupropion; however, a few persisted.
- More likely than other antidepressants to cause weight loss; however, may also cause weight gain in some people.
- May increase blood pressure. Blood pressure should be taken on treatment initiation and monitored periodically.
- The dosage of bupropion requires adjusting in kidney and liver disease.
- May not be suitable for some people including those with seizure disorders; eating disorders; undergoing alcohol, anticonvulsant, barbiturate, or benzodiazepine withdrawal; at risk of glaucoma; pregnant or breastfeeding; or taking monoamine oxidase inhibitors.
- As with other antidepressants, bupropion may increase the risk of suicidal thoughts or behavior. The risk is greatest for children and young adults under the age of 24. Monitor for worsening mood.
- May increase the risk of seizures. This risk is increased with higher dosages of bupropion, in those with head injuries or taking other medications which also lower the seizure threshold.
- May cause allergic reactions in some people with symptoms such as itchiness, facial swelling, and hives (urticaria). Stop treatment immediately and seek medical help.
- May cause a discontinuation syndrome if abruptly stopped or interrupted (symptoms include nausea, vomiting, diarrhea, headaches, dizziness, sweating, chills, tremors, vivid dreams, and insomnia).
- May interact with other drugs, such as other antidepressants; antipsychotics; agents that affect the electrical conductivity in the heart; those that induce or inhibit hepatic enzymes CYP2B6 or are metabolized by CYP2D6; other drugs that increase dopamine; or those that increase bleeding risk.
- Interaction with other medicines that increase serotonin levels (such as tramadol, other antidepressants, St John's wort) or overdosage may cause serotonin syndrome (symptoms include mental status changes [such as agitation, hallucinations, coma, delirium], fast heart rate, dizziness, flushing, muscle tremor or rigidity and stomach symptoms [such as nausea, vomiting, diarrhea]).
- Rare cases of priapism (painful erections more than 6 hours in duration) have been reported.
- May cause false-positive results on urine screening tests for amphetamines.
Notes: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. For a complete list of all side effects, click here.
- Can be taken with or without food.
- Avoid taking the last dose of the day after 5pm to minimize the risk of insomnia. At least eight hours should separate twice daily dosings of bupropion, and at least six hours should separate three times daily dosings of bupropion. Take bupropion exactly as directed by your doctor.
- Regardless of whether bupropion is being used as an antidepressant or as a smoking cessation aid, it should be started at a low dose and tapered up slowly over several days. Your doctor will advise you how to do this. Controlled-release forms of bupropion should be swallowed whole. Do not crush, divide, or chew because this may increase the risk of adverse effects including seizures.
- Zyban contains the same active ingredient as Wellbutrin, which is bupropion, and the two should never be used together.
- Bupropion may affect your judgment and your ability to drive or operate machinery. Avoid performing hazardous tasks such as driving if bupropion has this effect on you.
- If you are using bupropion as an aid to stopping smoking, start treatment while you are still smoking, and at least one week (maximum of two weeks) before your planned quit day, to ensure that the concentration of bupropion in your body is at an effective level. You should aim for complete abstinence (no smoking at all passed your quit day).
- If you have been taking bupropion for 7 to 12 weeks and have still not quit smoking, it is unlikely you will do so, and you should talk to your doctor about discontinuing it and reassessing other treatment options. However, some people may benefit from more than 12 weeks of bupropion treatment. In addition to bupropion treatment for smoking cessation, counseling and other support to help you quit the habit is important. Do not be discouraged if your first attempt at quitting smoking fails. Studies have estimated it may take up to 30 attempts for some smokers to successfully quit. Try again when conditions are more favorable.
- When used to treat Seasonal Affective Disorder (SAD), bupropion should be initiated in the autumn before the onset of depressive symptoms, continued throughout the winter season, and tapered off in early spring.
- Be alert for changes in behavior or mood including agitation, depression, or suicide-related events. Seek immediate medical advice if any changes are apparent.
- Stop taking bupropion if any symptoms suggestive of an allergic reaction occur (such as itchiness, body rash, swelling) and seek immediate medical help.
- See your doctor immediately if you develop any eye pain, visual disturbances, or swelling or redness around the eye.
- If using bupropion for depression, do not stop abruptly unless on a doctor's advice or if an allergic reaction occurs. If you need to discontinue bupropion, your doctor will advise you how to do so slowly.
- Minimize or avoid consumption of alcohol as your tolerance to it may be diminished while taking bupropion, and it may also increase the risk of neuropsychiatric adverse events.
- Talk to your doctor or pharmacist before you take any other medication with bupropion, including that bought over-the-counter.
6. Response and Effectiveness
- When bupropion is used for depression, improvements in sleep, energy, or appetite may be apparent within the first 1-2 weeks. Depressed mood or motivation may take up to 6-8 weeks to fully improve.
- Bupropion decreases nicotine cravings and withdrawal symptoms but effects take about one to two weeks to develop.
- Bupropion is metabolized to three active metabolites once in the body, each with varying durations of action.
- Bupropion [Package Insert]. Revised 09/2018. Alvogen Inc https://www.drugs.com/pro/bupropion.html
- Zyban (bupropion) (Package Insert). Revised 05/2017. GlaxoSmithKline LLC https://www.drugs.com/pro/zyban.html
- Aplenzin (bupropion) (Package Insert). Revised 05/2017. Valeant Pharmaceuticals North America LLC https://www.drugs.com/pro/aplenzin.html
- Wellbutrin (bupropion) (Package Insert). Revised 07/2018. GlaxoSmithKline LLC https://www.drugs.com/pro/wellbutrin.html
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use bupropion only for the indication prescribed.
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